Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) Infantum

Frontiers in Veterinary Science

Andrea T. Arantes¹  Aline N. Nascimento²  Monique R. Costa²  Mirela I. Sairre²  Ademar A. da Silva Filho³  Ana Carolina B. B. Candido⁴  Rodrigo C. S. Veneziani⁴  Sérgio R. Ambrósio⁴  Julia M. Souza⁴  Érica A. A. de Carvalho⁴  Renato L. T. Parreira⁴  Maria Fernanda da Silva⁵  Rafael P. de Mendonça⁵  Fernanda G. G. Dias⁵  Lizandra G. Magalhães⁵ 

[1] Centro Tecnológico Agropecuário, Batatais, Brazil;Centro de Ciências Naturais e Humanas, Universidade Federal Do ABC, Santo André, Brazil;Departamento de Ciências Farmacêuticas, Universidade Federal de Juiz de Fora, Juiz de Fora, Brazil;Núcleo de Pesquisa em Ciências Exatas e Tecnológica, Universidade de Franca, Franca, Brazil;Pós Graduação em Ciência Animal, Universidade de Franca, Franca, Brazil;

关键词: cutaneous leishmaniasis;    visceral leishmaniasis;    canine visceral leishmaniasis;    licochalcone A;    leishmanicidal activity;   

DOI  :  10.3389/fvets.2020.00527

来源: DOAJ

【 摘 要 】

The efficacy of Licochalcone A (LicoA) and its two analogs were reported against Leishmania (Leishmania) amazonensis and Leishmania (Leishmania) infantum in vitro, and in experimental model of L. (L.) infantum in vitro. Initially, LicoA and its analogs were screened against promastigote forms of L. (L.) amazonensis. LicoA was the most active compound, with IC50 values of 20.26 and 3.88 μM at 24 and 48 h, respectively. Against amastigote forms, the IC50 value of LicoA was 36.84 μM at 48 h. In the next step, the effectivity of LicoA was evaluated in vitro against promastigote and amastigote forms of L. (L.) infantum. Results demonstrated that LicoA exhibited leishmanicidal activity in vitro against promastigote forms with IC50 values of 41.10 and 12.47 μM at 24 and 48 h, respectively; against amastigote forms the IC50 value was 29.58 μM at 48 h. Assessment of cytotoxicity demonstrated that LicoA exhibited moderate mammalian cytotoxicity against peritoneal murine macrophages; the CC50 value was 123.21 μM at 48 h and showed about 30% of hemolytic activity at concentration of 400 μM. L. (L.) infantum-infected hamsters and treated with LicoA at 50 mg/kg for eight consecutive days was able to significantly reduce the parasite burden in both liver and spleen in 43.67 and 39.81%, respectively, when compared with negative control group. These findings suggest that chalcone-type flavonoids can be a promising class of natural products to be considered in the search of new, safe, and effective compounds capable to treat canine visceral leishmaniosis (CVL).

【 授权许可】

Unknown